Development of extended-voyaging anti-oxidant Linked Amphiphilic Polymeric Nanomicelles for Anti-Tuberculosis Drug Delivery

Amphiphilic chitosan-graft-poly(caprolactone)/(ferulic acid) (CS-g-PCL/FA) multi-co-polymers were fabricated by microwave-assisted ring opening polymerization followed by an 1-ethyl-3-(3-dimethyl-aminopropyl) carbodiimide (EDC)-mediated coupling reaction and characterized by Fourier transformed infr...

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Bibliographic Details
Published in:International journal of pharmaceutics 2017-05, Vol.524 (1-2), p.168-177
Main Authors: Praphakar, Rajendran Amarnath, Munusamy, Murugan A., Rajan, Mariappan
Format: Article
Language:English
Subjects:
A549 Cells
Antioxidants - chemistry
Chitosan
Drug Carriers - chemistry
Drug Compounding
Ferulic acid
Humans
Micelles
Nanoparticles - chemistry
Poly caprolactone
Polymers
Rifampicin
Self assembles
Tuberculosis - drug therapy
X-Ray Diffraction
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Summary:Amphiphilic chitosan-graft-poly(caprolactone)/(ferulic acid) (CS-g-PCL/FA) multi-co-polymers were fabricated by microwave-assisted ring opening polymerization followed by an 1-ethyl-3-(3-dimethyl-aminopropyl) carbodiimide (EDC)-mediated coupling reaction and characterized by Fourier transformed infrared (FTIR) spectroscopy. Graft copolymers self-assembled into nanomicelles, and were able to incorporate rifampicin (RF) into their hydrophobic inner cores. X-ray diffraction (XRD) patterns were applied to characterize the crystal structures of graft polymers and the effects of RF on micelle morphology. Empty and RF-loaded CS-g-PCL/FA nanomicelles underwent swelling and degradation in acidic pH conditions. Scanning electron microscopy, transmission electron microscopy, and dynamic light scattering revealed that the self-assembled, RF-loaded micelles were spherical, with an average size of 100–210nm. An in vitro study conducted at 37°C demonstrated that RF and FA release from micelles at pH 5.3 was much faster than that at pH 7.4. The RF and FA release was significantly accelerated by switching to an acidic pH, owing to swelling of the micelles at lower pH values caused by the rapid degradation of ester and amide bonds present in the micelles. Fluorescence micrographs revealed successful entry of the polymeric micelles into A549cell lines. Thus, graft polymeric micelles have promising potential for delivery of hydrophobic antitubercular drugs and may improve therapeutic approaches for tuberculosis.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2017.03.089